Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives

doi:10.6023/cjoc201308017

Chin. J. Org. Chem. ›› 2013, Vol. 33 ›› Issue (12): 2588-2595.DOI: 10.6023/cjoc201308017 Previous Articles Next Articles

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1-甲基-1,2,3,4-四氢异喹啉衍生物的合成及抗日本血吸虫活性评价

王文龙^a,b, 宋丽君^c, 王古平^a, 范文华^b, 殷旭仁^c, 余传信^c, 冯柏年^a,b

a 江南大学药学院无锡 214122;
b 江苏艾凡生物医药有限公司无锡 214122;
c 江苏省寄生虫病防治研究所无锡 214064

收稿日期:2013-08-14 修回日期:2013-09-28 发布日期:2013-10-10
通讯作者: 冯柏年，余传信 E-mail:fengbainian@jiangnan.edu.cn；chxnyu@163.com
基金资助:
国家自然科学基金(No. 30972581)、江苏省自然科学基金(No. BK2008110)、江苏省兴卫工程平台(No. ZX201108)和中央高校基本科研业务费(No. JUSRP1040)资助项目.

Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives

Wang Wenlong^a,b, Song Lijun^c, Wang Guping^a, Fan Wenhua^b, Yin Xuren^c, Yu Chuanxin^c, Feng Bainian^a,b

a School of Pharmaceutical Science, Jiangnan University, Wuxi 214122;
b Jiangshu Alpha Biopharmaceuticals, Inc., Wuxi 214122;
c Jiangsu Institute of Parasitic Diseases, Wuxi 214064

Received:2013-08-14 Revised:2013-09-28 Published:2013-10-10
Supported by:
Project supported by the National Natural Science Foundation of China (No. 30972581), the Natural Science Foundation of Jiangsu Province (No. BK2008110), the Health Promotion Project Foundation of Jiangsu Province (No. ZX201108), and the Fundamental Research Funds for the Central Universities (No. JUSRP1040).

Due to widespread and intensive use of antischistosomal drug, praziquantel (PZQ), there is serious concern that drug-resistant mutants of the parasite may emerge. To develop novel antischistosomal agents, a series of 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives were designed, synthesized, and evaluated for their antischistosomal activity against S. japonicum in vitro. The results indicated that compound 10 with chloroacetyl group showed better antischistosoaml activity than PZQ.

Key words: praziquantel, 1-methyl-1,2,3,4-tetrahydroisoquinoline derivatives, Schistosoma japonicum, antischistosomal activity

Cite this article

Wang Wenlong, Song Lijun, Wang Guping, Fan Wenhua, Yin Xuren, Yu Chuanxin, Feng Bainian. Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives[J]. Chin. J. Org. Chem., 2013, 33(12): 2588-2595.

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1-甲基-1,2,3,4-四氢异喹啉衍生物的合成及抗日本血吸虫活性评价

Synthesis and Evaluation of the Antischistosomal Activity against S. japonicum of 1-Methyl-1,2,3,4-tetrahydroisoquinoline Derivatives

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